Receptor Downregulation - How To Reset?

[dookie]

@Constatine , @haidut

I know there's been some talk recently about "receptors" being "downregulated", for example "dopamine receptor down regulation".

I have noticed after consuming a moderate-high amount of coffee, that it seems to produce less and less beneficial effects over the last few weeks. It is like I "feel" it less and less. Its bloating reducing, mood enhancing, androgenic effects diminish over time. Also, apathy has developed more and more. Are the dopamine receptors "down-regulated" in my case?

I know Constatine has recommended avoiding masturbation, and using memantine, to "reset" the dopamine sensitivity. Are there other approaches?

When the dopamine sensitivity is restored, and the receptors are "up-regulated", will caffeine give me the nice vibes again, even in low doses (as it used to)?

 

[haidut]

@Constatine , @haidut

I know there's been some talk recently about "receptors" being "downregulated", for example "dopamine receptor down regulation".

I have noticed after consuming a moderate-high amount of coffee, that it seems to produce less and less beneficial effects over the last few weeks. It is like I "feel" it less and less. Its bloating reducing, mood enhancing, androgenic effects diminish over time. Also, apathy has developed more and more. Are the dopamine receptors "down-regulated" in my case?

I know Constatine has recommended avoiding masturbation, and using memantine, to "reset" the dopamine sensitivity. Are there other approaches?

When the dopamine sensitivity is restored, and the receptors are "up-regulated", will caffeine give me the nice vibes again, even in low doses (as it used to)?

Caffeine desensitization is very well known, both anecdotally and clinically. The mechanism is not well know. However, using the chemical theacrine, which is very similar to caffeine was shown to produce all the mental/cognitive benefits of caffeine without sensitization and the best dose was 200mg daily. Higher doses did not produce more benefit and were better than even 800g caffeine daily. So, you can try to find some of that, it is available online but is much more expensive than caffeine.

 

[dookie]

@haidut - thank you for the advice. Do you have any personal experience with this "theacrine"? Does it feel similar to caffeine? It seems to be a mostly sport thing, included in some sports formulas, and most people mention it as "workout booster".

 

[Dante]

@Constatine , @haidut

I know there's been some talk recently about "receptors" being "downregulated", for example "dopamine receptor down regulation".

I have noticed after consuming a moderate-high amount of coffee, that it seems to produce less and less beneficial effects over the last few weeks. It is like I "feel" it less and less. Its bloating reducing, mood enhancing, androgenic effects diminish over time. Also, apathy has developed more and more. Are the dopamine receptors "down-regulated" in my case?

I know Constatine has recommended avoiding masturbation, and using memantine, to "reset" the dopamine sensitivity. Are there other approaches?

When the dopamine sensitivity is restored, and the receptors are "up-regulated", will caffeine give me the nice vibes again, even in low doses (as it used to)?

I don't think there is a relation with masturbation and dopamine receptor downregulation,it's more with unending ,escalating novelty of high speed internet porn (Gary wilson makes sure of this fact in his articles). As a rule of thumb, simply leave the activity for a few days/weeks which is causing desensitization( though it would be a massive exercise of discipline)

 

[haidut]

@haidut - thank you for the advice. Do you have any personal experience with this "theacrine"? Does it feel similar to caffeine? It seems to be a mostly sport thing, included in some sports formulas, and most people mention it as "workout booster".

Yep, I actually like theacrine more than caffeine. The 200mg dose does seem optimal.

 

[InChristAlone]

This is why I'm sticking with no caffeine. Or very irregular use. You could try not drinking it everyday. Be aware though that breaking the addiction is hard once you've become adapted. I still feel like my brain is recovering 5 weeks later. I do love waking up in the morning and not needing it for energy.

 

[dookie]

@haidut

Do you think a drug like cyproheptadine would "reset" the dopamine receptor sensitivity? I understand that it increases "receptor density" of serotonin, so the body is more sensitive to serotonin. Does it do this for dopamine as well? Could it in this sense re-sensitize one to caffeine and other dopaminergic drugs?

 

[haidut]

@haidut

Do you think a drug like cyproheptadine would "reset" the dopamine receptor sensitivity? I understand that it increases "receptor density" of serotonin, so the body is more sensitive to serotonin. Does it do this for dopamine as well? Could it in this sense re-sensitize one to caffeine and other dopaminergic drugs?

Given that cypro is an antagonist at D3 in relevant concentrations it should increase receptor density there. Antagonist at D1 and D2 happens at too high doses to be clinically relevant unless you are taking 32mg+ daily.

 

[ddjd]

Yep, I actually like theacrine more than caffeine. The 200mg dose does seem optimal.

Does it offer all of the other benefits of caffeine that ray talks about

 

[ddjd]

using memantine, to "reset" the dopamine sensitivity. Ar

Is this true? Any success as of yet?

 

[Frankdee20]

Caffeine isn’t directly agonizing Dopamine, so I don’t think it’s downregulating that. It’s antagonizing GABA, but simultaneously upregulating it. It’s primarily effecting adenosine, and whatever impedes adenosine, allows cetacholamines to work better.

 

[ddjd]

Chromium has also been shown to lower the cortisol response to challenge
with 5-hydroxy-L-tryptophan (5-HTP) and decrease the sensitivity of 5-HT
2A receptors
(Attenburrow et al 2002).

 

[haidut]

Does it offer all of the other benefits of caffeine that ray talks about

I think so. I asked Ray about it years ago and he said it would be good alternative to caffeine but that he prefers coffee to supplements.

 

[Ron J]

I'm curious about this. I take dopamine agonists, and I'm wondering if there's a way to prevent the drop in sensitivity or downregulation, other than cycling on and off.